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Design, synthesis and anticancer activity of N-(1-(4-(dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)-1-oxo-3-phenylpropan-2-yl derivatives
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2017-07-11 , DOI: 10.1016/j.bmcl.2017.07.029
Mura Reddy Gudisela , N. Srinivasu , Chaitanya Mulakayala , Praveen Bommu , M.V. Basaveswara Rao , Naveen Mulakayala

Novel N-(1-(4-(dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)-1-oxo-3-phenylpropan-2-yl derivatives were designed, synthesized and their chemical structures were confirmed by 1H NMR, 13C NMR and Mass spectra. The anticancer activities of the newly synthesized compounds were evaluated in vitro against three human cancer cell lines including K562, Colo-205 and MDA-MB 231 by MTT assay. The screening results showed that five compounds (16b, 16d, 16i, 16p and 16q) exhibited potent cytotoxic activities with IC50 values between 20 and 40 μM. Further in vitro studies revealed that inhibition of sirtuins could be the possible mechanism of action of these molecules.



中文翻译:

N-(1-(4-(二苯并[ bf ] [1,4]噻嗪平-11-基)哌嗪-1-基)-1-氧代-3-苯基丙烷-2-的设计,合成及抗癌活性yl衍生物

设计,合成了新型的N-(1-(4-(二苯并[ bf ] [1,4]噻嗪pin-11-基)哌嗪-1-基)-1-氧代-3-苯基丙烷-2-基衍生物并通过1 H NMR,13 C NMR和质谱证实了它们的化学结构,并通过MTT法体外评估了新合成的化合物对三种人类癌细胞株K562,Colo-205和MDA-MB 231的抗癌活性。筛选结果表明,5种化合物(16b16d16i16p16q)表现出强烈的细胞毒性活性,IC 50为50。值介于20和40μM之间。进一步的体外研究表明,抑制沉默调节蛋白可能是这些分子起作用的可能机制。

更新日期:2017-07-11
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